JP7004459B2 - 神経変性疾患の治療に用いるｌｒｒｋ２阻害剤としてのピリミジン－２－イルアミノ－１ｈ－ピラゾール - Google Patents
神経変性疾患の治療に用いるｌｒｒｋ２阻害剤としてのピリミジン－２－イルアミノ－１ｈ－ピラゾール Download PDFInfo
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- JP7004459B2 JP7004459B2 JP2018565694A JP2018565694A JP7004459B2 JP 7004459 B2 JP7004459 B2 JP 7004459B2 JP 2018565694 A JP2018565694 A JP 2018565694A JP 2018565694 A JP2018565694 A JP 2018565694A JP 7004459 B2 JP7004459 B2 JP 7004459B2
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- 0 *c1c(Nc2ncc(*)c(*)n2)[n](*)nc1* Chemical compound *c1c(Nc2ncc(*)c(*)n2)[n](*)nc1* 0.000 description 14
- MDELZHGRFDBKDV-QQSLQFIPSA-N CCNc1nc(N/C(/NC2CC2)=C/C([C@@H](C2)[C@@H]2C#N)=N)ncc1C(F)(F)F Chemical compound CCNc1nc(N/C(/NC2CC2)=C/C([C@@H](C2)[C@@H]2C#N)=N)ncc1C(F)(F)F MDELZHGRFDBKDV-QQSLQFIPSA-N 0.000 description 1
- LXRVHITUSDCRCT-UHFFFAOYSA-N CCNc1nc(Nc2cc(C(C)(CCO3)C3=O)n[n]2C2CC2)ncc1C(F)(F)F Chemical compound CCNc1nc(Nc2cc(C(C)(CCO3)C3=O)n[n]2C2CC2)ncc1C(F)(F)F LXRVHITUSDCRCT-UHFFFAOYSA-N 0.000 description 1
- OJRGUSSBPATGEO-UHFFFAOYSA-N CCNc1nc(Nc2cc(C)n[n]2C2CC2)ncc1C(F)(F)F Chemical compound CCNc1nc(Nc2cc(C)n[n]2C2CC2)ncc1C(F)(F)F OJRGUSSBPATGEO-UHFFFAOYSA-N 0.000 description 1
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- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
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- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
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- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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- C07B59/00—Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
- C07B59/002—Heterocyclic compounds
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- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
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- C07—ORGANIC CHEMISTRY
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- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
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- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
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- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
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- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
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- C07D487/04—Ortho-condensed systems
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/12—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains three hetero rings
- C07D491/20—Spiro-condensed systems
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- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—Ortho-condensed systems
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
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- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Psychology (AREA)
- Rheumatology (AREA)
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- Hospice & Palliative Care (AREA)
- Pain & Pain Management (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Epidemiology (AREA)
- Hematology (AREA)
- Immunology (AREA)
- Oncology (AREA)
- Dermatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicinal Preparation (AREA)
- Management, Administration, Business Operations System, And Electronic Commerce (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (9)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662350876P | 2016-06-16 | 2016-06-16 | |
| US62/350,876 | 2016-06-16 | ||
| US201662417151P | 2016-11-03 | 2016-11-03 | |
| US62/417,151 | 2016-11-03 | ||
| US201762476581P | 2017-03-24 | 2017-03-24 | |
| US62/476,581 | 2017-03-24 | ||
| US201762510711P | 2017-05-24 | 2017-05-24 | |
| US62/510,711 | 2017-05-24 | ||
| PCT/US2017/037782 WO2017218843A1 (en) | 2016-06-16 | 2017-06-15 | Pyrimidin-2-ylamino-1h-pyrazols as lrrk2 inhibitors for use in the treatment of neurodegenerative disorders |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019521984A JP2019521984A (ja) | 2019-08-08 |
| JP2019521984A5 JP2019521984A5 (enrdf_load_stackoverflow) | 2020-07-30 |
| JP7004459B2 true JP7004459B2 (ja) | 2022-02-10 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018565694A Active JP7004459B2 (ja) | 2016-06-16 | 2017-06-15 | 神経変性疾患の治療に用いるｌｒｒｋ２阻害剤としてのピリミジン－２－イルアミノ－１ｈ－ピラゾール |
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Families Citing this family (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2017087905A1 (en) | 2015-11-20 | 2017-05-26 | Denali Therapeutics Inc. | Compound, compositions, and methods |
| US11028080B2 (en) | 2016-03-11 | 2021-06-08 | Denali Therapeutics Inc. | Substituted pyrimidines as LRKK2 inhibitors |
| PE20190395A1 (es) | 2016-06-16 | 2019-03-13 | Denali Therapeutics Inc | Pirimidin-2-ilamino-1h-pirazoles como inhibidores de lrrk2 para el uso en el tratamiento de trastornos neurodegenerativos |
| EP3717473B1 (en) * | 2017-11-21 | 2024-01-10 | Denali Therapeutics Inc. | Polymorphs and solid forms of a pyrimidinylamino-pyrazole compound, and methods of production |
| ES2975958T3 (es) | 2017-12-20 | 2024-07-18 | Denali Therapeutics Inc | Procedimiento para la preparación de compuestos de pirimidinil-4-aminopirazol |
| KR20190131981A (ko) * | 2018-05-18 | 2019-11-27 | 재단법인 대구경북첨단의료산업진흥재단 | 외상성 뇌손상 또는 뇌졸중의 예방 또는 치료용 약학적 조성물 |
| AR118641A1 (es) | 2019-04-11 | 2021-10-20 | Denali Therapeutics Inc | Compuestos, composiciones y métodos |
| EA202193285A1 (ru) * | 2019-05-31 | 2022-03-04 | Денали Терапьютикс Инк. | Состав с модифицированным высвобождением соединения пиримидиниламинопиразола и способы лечения |
| EP3769768A1 (en) | 2019-07-23 | 2021-01-27 | Consejo Superior de Investigaciones Cientificas (CSIC) | Compounds useful for the treatment of parkinson s disease |
| JP2023501949A (ja) * | 2019-10-29 | 2023-01-20 | バイオジェン・エムエイ・インコーポレイテッド | スピロ環ｏ－糖タンパク質－２－アセトアミド－２－デオキシ－３－ｄ－グルコピラノシダーゼ阻害剤 |
| KR102342803B1 (ko) | 2020-03-23 | 2021-12-24 | 환인제약 주식회사 | 신규한 피리미딘 유도체 및 이를 포함하는 신경퇴행성 질환 및 암의 예방 또는 치료용 조성물 |
| JP7671775B2 (ja) | 2020-03-23 | 2025-05-02 | ファニン ファーマシューティカル カンパニー リミテッド | 新規なピリミジン誘導体及びこれを含む神経退行性疾患及び癌の予防又は治療用組成物 |
| KR20230091150A (ko) * | 2020-10-29 | 2023-06-22 | 수저우 야바오 파마슈티걸 알앤디 컴퍼니 리미티드 | 치환된 디아릴아민 화합물 및 이의 약학적 조성물, 제조 방법과 용도 |
| CN117769422A (zh) * | 2021-04-30 | 2024-03-26 | 戴纳立制药公司 | 治疗与监测帕金森病的方法 |
| JP2024541934A (ja) | 2021-10-27 | 2024-11-13 | ハー・ルンドベック・アクチエゼルスカベット | Ｌｒｒｋ２阻害剤 |
| MX2024007383A (es) | 2021-12-15 | 2024-08-28 | Whan In Pharmaceutical Co Ltd | Derivado de pirimidina macrocíclica, método para preparar el mismo y composición farmacéutica para prevención o tratamiento de una enfermedad neurodegenerativa que contiene el mismo como ingrediente activo. |
| WO2024056775A1 (en) | 2022-09-15 | 2024-03-21 | H. Lundbeck A/S | Macrocyclic leucine-rich repeat kinase 2 (lrrk2) inhibitors |
| TW202434570A (zh) | 2022-11-03 | 2024-09-01 | 美商戴納立製藥公司 | 嘧啶三唑化合物之固體及共晶體形式 |
| CN115894456A (zh) * | 2022-11-13 | 2023-04-04 | 药康众拓(江苏)医药科技有限公司 | 一种氘代吡唑氨基嘧啶类化合物、药物组合物和用途 |
| AU2023385721A1 (en) | 2022-11-22 | 2025-05-22 | Denali Therapeutics Inc. | Processes and intermediates for the preparation of a pyrimidine aminopyrazole compound |
| CN115819405A (zh) * | 2022-12-20 | 2023-03-21 | 沪渝人工智能研究院 | 嘧啶氨基吡唑衍生物及其作为富亮氨酸重复激酶2抑制剂的应用 |
| WO2025051214A1 (zh) * | 2023-09-07 | 2025-03-13 | 上海翊石医药科技有限公司 | 一种芳杂环类化合物及其制备方法 |
| CN118878521B (zh) * | 2024-09-26 | 2025-02-14 | 苏州美诺医药科技有限公司 | 一种lrrk2抑制剂的制备方法 |
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| WO2009127642A2 (en) | 2008-04-15 | 2009-10-22 | Cellzome Limited | Use of lrrk2 inhibitors for neurodegenerative diseases |
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